Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.

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Bridoux A, Millet R, Pommery J, Pommery N, Henichart JP

Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.

Bioorg Med Chem. 2010 Jun 1;18(11):3910-24. doi: 10.1016/j.bmc.2010.04.034. Epub 2010 Apr 18.

PubMed ID
20451397 [ View in PubMed
]
Abstract

Research on dual inhibitors of both 5-LOX and COXs gained interest due to the overexpressions of these enzymes during the malignant state of the evolution of prostate cancer. In order to take part in this research, new N-aroyl-tetrahydro-gamma-carbolines issued from the modification of Indomethacin have been synthesised. As for the NSAIDs, the compounds have been tested for their activity against COX(1), COX(2) plus against 5-LOX and against the proliferation of malignant prostate cancer. Interesting cytotoxic activities and selectivities of some tetrahydro-gamma-carboline derivatives have been obtained.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
CelecoxibProstaglandin G/H synthase 2IC 50 (nM)800N/AN/ADetails
IndomethacinProstaglandin G/H synthase 1IC 50 (nM)200N/AN/ADetails
IndomethacinProstaglandin G/H synthase 1IC 50 (nM)6000N/AN/ADetails
IndomethacinProstaglandin G/H synthase 2IC 50 (nM)500N/AN/ADetails
ZileutonArachidonate 5-lipoxygenaseIC 50 (nM)700N/AN/ADetails
ZileutonArachidonate 5-lipoxygenaseIC 50 (nM)800N/AN/ADetails